1n7j
From Proteopedia
(New page: 200px<br /> <applet load="1n7j" size="450" color="white" frame="true" align="right" spinBox="true" caption="1n7j, resolution 2.70Å" /> '''The structure of Ph...) |
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caption="1n7j, resolution 2.70Å" /> | caption="1n7j, resolution 2.70Å" /> | ||
'''The structure of Phenylethanolamine N-methyltransferase in complex with S-adenosylhomocysteine and an iodinated inhibitor'''<br /> | '''The structure of Phenylethanolamine N-methyltransferase in complex with S-adenosylhomocysteine and an iodinated inhibitor'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1N7J is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SAH and IDI as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Phenylethanolamine_N-methyltransferase Phenylethanolamine N-methyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.1.1.28 2.1.1.28] Full crystallographic information is available from [http:// | + | 1N7J is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SAH:'>SAH</scene> and <scene name='pdbligand=IDI:'>IDI</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Phenylethanolamine_N-methyltransferase Phenylethanolamine N-methyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.1.1.28 2.1.1.28] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1N7J OCA]. |
==Reference== | ==Reference== | ||
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[[Category: s-adenosylmethionine]] | [[Category: s-adenosylmethionine]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:27:34 2008'' |
Revision as of 14:27, 15 February 2008
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The structure of Phenylethanolamine N-methyltransferase in complex with S-adenosylhomocysteine and an iodinated inhibitor
Contents |
Overview
The crystal structures of human phenylethanolamine N-methyltransferase in, complex with S-adenosyl-l-homocysteine (7, AdoHcy) and either, 7-iodo-1,2,3,4-tetrahydroisoquinoline (2) or, 8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine (3, LY134046) were, determined and compared with the structure of the enzyme complex with 7, and 7-aminosulfonyl-1,2,3,4-tetrahydroisoquinoline (1, SK&F 29661). The, enzyme is able to accommodate a variety of chemically disparate functional, groups on the aromatic ring of the inhibitors through adaptation of the, binding pocket for this substituent and by subtle adjustments of the, orientation of the inhibitors within the relatively planar binding site., In addition, the interactions formed by the amine nitrogen of all three, inhibitors reinforce the hypothesis that this functional group mimics the, beta-hydroxyl of norepinephrine rather than the amine. These studies, provide further clues for the development of improved inhibitors for use, as pharmacological probes.
Disease
Known diseases associated with this structure: Hypertension, essential, 145500 (1) OMIM:[171190]
About this Structure
1N7J is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Phenylethanolamine N-methyltransferase, with EC number 2.1.1.28 Full crystallographic information is available from OCA.
Reference
Molecular recognition of sub-micromolar inhibitors by the epinephrine-synthesizing enzyme phenylethanolamine N-methyltransferase., McMillan FM, Archbold J, McLeish MJ, Caine JM, Criscione KR, Grunewald GL, Martin JL, J Med Chem. 2004 Jan 1;47(1):37-44. PMID:14695818
Page seeded by OCA on Fri Feb 15 16:27:34 2008
Categories: Homo sapiens | Phenylethanolamine N-methyltransferase | Single protein | Archbold, J. | Caine, J.M. | Criscione, K.R. | Grunewald, G.L. | Martin, J.L. | McLeish, M.J. | McMillan, F.M. | IDI | SAH | Adrenaline | Catecholamine | Epinephrine | Methyltransferase | S-adenolsylhomocysteine | S-adenosylmethionine
